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How Physicochemical Properties of Drugs Affect Their Metabolism and Clearance
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. (Drug Delivery)
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. (Drug delivery)ORCID iD: 289172612
2016 (English)In: New Horizons in Predictive Drug Metabolism and Pharmacokinetics / [ed] Alan G. E. Wilson, Cambridge: Royal Society of Chemistry, 2016, 1-26 p.Chapter in book (Refereed)
Abstract [en]

In this chapter the transport proteins and enzymes of importance for drug clearance are discussed. The primary organ for drug metabolism is the liver and to reach the intracellular compartment of hepatocytes, orally administered drugs must cross both the intestinal wall and the cell membrane of the liver cells. Transport proteins present in the cellular membrane may facilitate or hinder the compounds crossing these cellular barriers and hence will influence to what extent compounds will reach the enzymes. Here, the enzymes and transport proteins of importance for drug clearance are discussed. The molecular features of importance for drug interactions with transport proteins and enzymes are analyzed and the possibility to predict molecular features vulnerable to enzymatic degradation is discussed. From detailed analysis of the current literature it is concluded that for interaction, both with transport proteins and enzymes, lipophilicity plays a major role. In addition to this property, molecular properties such as hydrogen bond acceptors and donors, charge, aromaticity and molecular size can be used to distinguish between routes of clearance.

Place, publisher, year, edition, pages
Cambridge: Royal Society of Chemistry, 2016. 1-26 p.
Series
RSC Drug Discovery Series, ISSN 2041-3203 ; 49
National Category
Pharmaceutical Sciences
Research subject
Pharmacokinetics and Drug Therapy
Identifiers
URN: urn:nbn:se:uu:diva-288002DOI: 10.1039/9781782622376-00001Scopus ID: 2-s2.0-84952641815ISBN: 978-1-84973-828-6 (print)ISBN: 978-1-78262-237-6 (print)OAI: oai:DiVA.org:uu-288002DiVA: diva2:923714
Available from: 2016-04-27 Created: 2016-04-27 Last updated: 2017-01-02Bibliographically approved

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CiteExportLink to record
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